Bioorganic & Medicinal Chemistry Letters 2004-01-19

Synthesis of novel melanocortin 4 receptor agonists and antagonists containing a succinamide core.

Ning Xi, Clarence Hale, Michael G Kelly, Mark H Norman, Markian Stec, Shimin Xu, James W Baumgartner, Christopher Fotsch

Index: Bioorg. Med. Chem. Lett. 14 , 377, (2004)

Full Text: HTML

Abstract

A novel series of piperazines appended to a succinamide backbone were synthesized and found to have a high affinity for the melanocortin-4 receptor (IC(50)s ranging from <0.1 to 200 nM). Both agonists and antagonists of MC4R were prepared by modifying the groups attached to the right-hand side of the succinamide. This series also exhibits a high level of selectivity (up to 7000-fold) over mouse MC1R and human MC3R.